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Naquotinib

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Chemical Structure| 1448232-80-1 同义名 : ASP8273
CAS号 : 1448232-80-1
货号 : A327192
分子式 : C30H42N8O3
纯度 : 99%+
分子量 : 562.706
MDL号 : MFCD30496701
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(186.6 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1
描述 Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR[1]. Naquotinib is noted for its capability to inhibit the proliferation of cells endogenously dependent on EGFR, affecting the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M), and PC-9ER(del ex19/T790M) with IC50 values ranging from 8 to 33 nM[1]. It specifically targets the phosphorylation of EGFR and its downstream signaling pathways, ERK and Akt, starting from concentrations as low as 10 nM in HCC827 and NCI-H1975 cells, with inhibition effects visible at 1000 nM in A431 cells. In NCI-H1650 (del ex19), Naquotinib curtails cell growth with an IC50 of 70 nM, showcasing effectiveness where other EGFR-TKIs have limited impact[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.77mL

3.55mL

1.78mL
参考文献

[1]Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of t

[2]Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Ph